Product Details of 39901-94-5. The protonation of heteroatoms in aromatic heterocycles can be divided into two categories: lone pairs of electrons are in the aromatic ring conjugated system; and lone pairs of electrons do not participate. Compound: Picolinoyl chloride hydrochloride, is researched, Molecular C6H5Cl2NO, CAS is 39901-94-5, about A new pathway via intermediate 4-amino-3-fluorophenol for the synthesis of regorafenib. Author is Du, Fangyu; Zhou, Qifan; Shi, Yajie; Yu, Miao; Sun, Wenjiao; Chen, Guoliang.
A practical synthetic route to regorafenib, in which the target compound was obtained via a 10-step synthesis starting from 2-picolinic acid, 4-chloro-3-(trifluoromethyl)aniline and 3-fluorophenol was reported. Crucial to the strategy was the preparation of 4-amino-3-fluorophenol via Fries and Beckman rearrangements using an economical and practical protocol. The main advantages of the route include inexpensive starting materials and an acceptable overall yield. A scale-up experiment was carried out to provide regorafenib with 99.96% purity in 46.5% total yield.
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